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Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 311.72. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.21 mL||16.04 mL||32.08 mL|
|5 mM||0.64 mL||3.21 mL||6.42 mL|
|10 mM||0.32 mL||1.6 mL||3.21 mL|
|50 mM||0.06 mL||0.32 mL||0.64 mL|
References are publications that support the biological activity of the product.
Hurst et al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066
Timmermann et al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074
Kalappa et al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819
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Keywords: PNU 120596, PNU 120596 supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, active, vivo, Nicotinic, Receptors, Acetylcholine, PNU120596, PAM, (a7), 2498, Tocris Bioscience
15 Citations for PNU 120596
Citations are publications that use Tocris products. Selected citations for PNU 120596 include:
Noviello et al (2021) Structure and gating mechanism of the α7 nicotinic acetylcholine receptor. Cell PMID: 33735609
Bali et al (2019) Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep 9 9324 PMID: 31249369
Gimenz-Gomez et al (2018) Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens. Neuropharmacology 135 581 PMID: 29705534
Pandya and Yakel (2013) Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT?a receptor antagonist. Neuropharmacology 70 35 PMID: 23321689
Barykin et al (2019) Isomerization of Asp7 in Beta-Amyloid Enhances Inhibition of the α7 Nicotinic Receptor and Promotes Neurotoxicity. Cells 8 PMID: 31349637
Pérez-Alvarez et al (2012) Pharmacological characterization of native α7 nicotinic ACh receptors and their contribution to depolarization-elicited exocytosis in human chromaffin cells. Br J Pharmacol 165 908 PMID: 21790533
David et al (2010) Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes. Eur J Neurosci 31 978 PMID: 20377613
Kasheverov et al (2015) 6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor. Mar Drugs 13 1255 PMID: 25775422
Thomsen et al (2015) α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties. PLoS One 10 e0130572 PMID: 26086615
John et al (2015) Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. PLoS One 1601 15 PMID: 25553616
Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. PLoS One 10 e0125116 PMID: 25906356
Zhang et al (2015) Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor. Mol Pharmacol 10 e0137588 PMID: 26340537
daCosta et al (2015) Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors. J Neurosci 6 8057 PMID: 26282895
Yamauchi et al (2012) Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. Nat Commun 82 687 PMID: 22784805
Maldifassi et al (2014) A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages. PLoS One 9 e108397 PMID: 25259522
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.